BMS202

製品コードS7912 バッチS791202

印刷

化学情報

 Chemical Structure Synonyms PD-1/PD-L1 inhibitor 2 Storage
(From the date of receipt)
3 years -20°C powder
1 years -80°C in solvent
化学式

C25H29N3O3

分子量 419.52 CAS No. 1675203-84-5
Solubility (25°C)* 体外 DMSO 83 mg/mL (197.84 mM)
Ethanol 83 mg/mL (197.84 mM)
Water Insoluble
体内 (毎回新しく調製した物を用意してください)
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution
5%DMSO 5%Tween80 90%ddH2O

この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。

1.100mg/ml (2.62mM) Taking the 1 mL working solution as an example, add 50 μL of 22 mg/ml clarified DMSO stock solution to 50 μL of Tween80, mix evenly to clarify; then continue to add 900 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O

この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。

2.000mg/ml (4.77mM) Taking the 1 mL working solution as an example, add 50 μL of 40 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液(一定の濃度)を調合する

生物活性

製品説明 BMS202 is a small-molecule PD-1/PD-L1 interaction inhibitor with IC50 of 18 nM.
in vitro

BMS-202 inhibits PD-1/PD-L1 binding in SCC-3 and Jurkat cells with IC50 of 15 μM and 10 μM, respectively.

in vivo

BMS-202 treatment shows a clear antitumor effect compared with the controls, in humanized MHC- dKO NOG mice.

プロトコル(参考用のみ)

細胞アッセイ 細胞株 SCC-3 and Jurkat cells
濃度 IC50 of 15 μM and 10 μM
反応時間 4 days
実験の流れ

Cells were treated with various concentrations of drug for 4 days.

動物実験 動物モデル NOG-dKO mice
投薬量 20 mg/kg
投与方法 i.p.

参考

  • https://patents.google.com/patent/WO2015034820A1
  • https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5058683/
  • https://pubmed.ncbi.nlm.nih.gov/31839668/

Selleckの高級品が、幾つかの出版された研究調査結果(以下を含む)で使われた:

Therapeutic potential of isochlorogenic acid A from Taraxacum officinale in improving immune response and enhancing the efficacy of PD-1/PD-L1 blockade in triple-negative breast cancer [ Front Immunol, 2025, 16:1529710] PubMed: 40109332
Metabolic profiling of glioblastoma and identification of G0S2 as a metabolic target [ Front Oncol, 2025, 15:1572040] PubMed: 40519301
Impact of the PD-1/PD-L1 inhibitor SCL-1 on MDA-MB231 tumor growth in a humanized MHC-double knockout NOG mouse model [ Sci Rep, 2025, 15(1):26918] PubMed: 40707559
In Vivo Antitumor Activity of the PD-1/PD-L1 Inhibitor SCL-1 in Various Mouse Tumor Models [ In Vivo, 2025, 39(1):80-95] PubMed: 39740910
Uncovering the colorectal cancer immunotherapeutic potential: Evening primrose (Oenothera biennis) root extract and its active compound oenothein B targeting the PD-1/PD-L1 blockade [ Phytomedicine, 2024, 125:155370] PubMed: 38266440
Development and In Vivo Evaluation of Small-Molecule Ligands for Positron Emission Tomography of Immune Checkpoint Modulation Targeting Programmed Cell Death 1 Ligand 1 [ J Med Chem, 2024, 67(5):4036-4062] PubMed: 38442487
Isolation and Total Synthesis of PM170453, a New Cyclic Depsipeptide Isolated from Lyngbya sp [ Mar Drugs, 2024, 22(7)303] PubMed: 39057411
Theoretical and experimental studies on the interaction of biphenyl ligands with human and murine PD-L1: Up-to-date clues for drug design [ Comput Struct Biotechnol J, 2023, 21:3355-3368] PubMed: 37384351
Turning a Tumor Microenvironment Pitfall into Opportunity: Discovery of Benzamidoxime as PD-L1 Ligand with pH-Dependent Potency [ Int J Mol Sci, 2023, 24(6)5535] PubMed: 36982608
Turning a Tumor Microenvironment Pitfall into Opportunity: Discovery of Benzamidoxime as PD-L1 Ligand with pH-Dependent Potency [ Int J Mol Sci, 2023, 24(6)5535] PubMed: 36982608

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。